1994 Fiscal Year Final Research Report Summary
Synthesis of Biologically Active Heterocyclic Compounds Labelled with Positron Emitting Radionuclides for Diagnoses of Diseases of Brain and Heart and Cancer
| Project/Area Number |
04454291
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| Research Category |
Grant-in-Aid for General Scientific Research (B)
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| Allocation Type | Single-year Grants |
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| Research Field |
Radiation science
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| Research Institution | Tohoku University |
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Principal Investigator |
TADA Masao Tohoku Univ.Inst.of Development, Aging and Cancer, Assoc.Prof., 加齢医学研究所, 助教授 (10006083)
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| Co-Investigator(Kenkyū-buntansha) |
FUJIWARA Takehiko Tohoku Univ., Cyclotron and Rl Center, Instr., サイクロトロンRIセンター, 助手 (70238632)
IWATA Ren Tohoku Univ., Cyclotron and RI Center, Assoc.Prof., サイクロトロンRIセンター, 助教授 (60143038)
KUBOTA Kazuo Tohoku Univ., Inst.of Development, Aging and Cancer, Assoc.Prof., 加齢医学研究所, 助教授 (40161674)
SUGIYAMA Hiroshi Tohoku Univ., Inst.for Chem.Res.Sci., Assoc.Prof., 反応化学研究所, 助教授 (90006304)
FUKUDA Hiroshi Tohoku Univ., Inst.of Development, Aging and Cancer, Prof., 加齢医学研究所, 教授 (30125645)
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| Project Period (FY) |
1992 – 1994
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| Keywords | Synthesis / [fluoroacetyl-^<18>F] Fluoromelatonin / [^<18>F] Fluoride / Cyclotron / Radioactive isotope / N^<omega>- [^<18>F] Fluoroacetylserotonin |
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| Research Abstract |
An efficient synthesis of [fluoroacetyl-^<18>F] fluoromelatonin (N^<omega>- [^<18>F] Fluoroacety1-5-methoxytryptamine) starting from [^<18>F]fluoride has been established. [^<18>F] Fluoride was produced by the ^<18>O (p, n)^<18>F nuclear reaction from a circulating 20%-enriched [^<18>O] water target using the Tohoku University Cyclotron. The ^<18>F nuclide thereby formed was converted to potassium [^<18>F] fluoride. The reaction of[^<18>F]fluoride with ethyl p-toluenesulfonyloxyacetate derived from ethyl bromoacetate with silver p-toluenesulfonate afforded ethyl [^<18>F] fluoroacetate, which was then hydrolyzed with alkali and condensed with 5-methoxytryptamine in the presence of dicyclohexylcarbodiimide to give the desired radioactive isotope in a 26.7% radiochemical yield. The purity, specific activity and the total time required for its synthesis are>98%, 540 mCi/mumol and ca.90 min, respectively.
N^<omega>- [^<18>F] Fluoroacetylserotonin was synthesized under similar conditions in 22.6% radiochemical yield. The purity and specific activity of the hormone are>98% and 600 mCi/mumol, respectively.
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Research Products
(6 results)
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[Publications] Masao Tada, Ren Iwata, Hiroshi Sugiyama, Kazunori Sato, Claudio Pascali, Hiroshi Fukuda, Kazuo Kubota, Roko Kubota, Hiromu Takahashi, Akira Wakui, Yoshinao Abe, Takehiko Fujiwara, Tachio Sato, and Tatsuo Ido: "A Rapid Synthesis of [fluoroacetyl-^<18>F]Fluoromelatonin (N^<omega>-[^<18>F]Fluoroacety1-5-methoxytryptamine), a Potential Diagnostic Imaging Agent" J.Labelled Compds.Radiopharm. 33. 601-606 (1993)
Description
「研究成果報告書概要(欧文)」より
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[Publications] Masao Tada, Ren Iwata, Hiroshi Sugiyama, Kazunori Sato, Hiroshi Fukuda, Kazuo Kubota, Roko Kubota, Hiromu Takahashi, Akira Wakui, Yoshinao Abe, Takehiko Fujiwara, Tachio Sato, and Tatsuo Ido: "A Rapid One-pot Synthesis of [fluoroacetyl-^<18>F] Fluoromelatonin" CYRIC Ann.Rep.1992. 117-121 (1993)
Description
「研究成果報告書概要(欧文)」より
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[Publications] Masao Tada, Ren Iwata, Hiroshi Sugiyama, Kazunori Sato, Hiroshi Fukuda, Kazuo Kubota, Roko Kubota, Takehiko Fujiwara, Hiromu Takahashi, Akira Wakui, and Tatsuo Ido: "An Efficient Synthesis of N^<omega>-[^<18>F]Fluoroacetylserotonin (N^<omega>-[^<18>F]Fluoroacety1-5-hydroxytryptamine)" J.Labelled Compds.Radiopharm. 34. 741-746 (1994)
Description
「研究成果報告書概要(欧文)」より
